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From the petroleum ether and ethyl acetate portions of the 95% ethanol extract of  Ficus tikoua  Bur., a new hemiacetal chromone racemate, named (±)-ficunomone ( 1 ), together with twenty-two known flavonoids ( 2 - 23 ) were isolated. The new structure was elucidated by NMR, HRESIMS, and X-ray single-crystal diffraction analysis, and the known structures were determined by comparison of spectroscopic data with those reported from literatures. All the compounds were assayed for their inhibitory activities against yeast  α -glucosidase, seven flavonoids could inhibit  α -glucosidase, among which compounds  22  and  23  exhibited the highest inhibitory activity, with IC 50  values at 5.12 ± 0.10 and 3.43 ± 0.15 μM respectively. Preliminary structure and relationship activity of all the compounds was analysed. Kinetic analysis of compounds  22  and  23  indicated that they are both uncompetitive inhibitors. Molecular docking studies revealed that they bound to amino acid residues of the  α -glucosidase activity pocket.

A new hemiacetal chromone racemate and α-glucosidase inhibitors from Ficus tikoua Bur